Hyaluronic acid coated poly(butyl cyanoacrylate) nanoparticles as anticancer drug carriers
Hyaluronic acid coated poly(butyl cyanoacrylate) nanoparticles as anticancer drug carriers
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DOI：
10.1016/j.ijpharm.2009.02.012
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发表时间：
2009-05-21
影响因子：
5.8
通讯作者：
Yin, Chunhua
中科院分区：
文献类型：
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作者：
He, Miao;Zhao, Ziming;Yin, Chunhua
在透明质酸（HA）存在下，通过铈离子引发氰基丙烯酸丁酯（BCA）自由基聚合，制备了透明质酸（HA）包覆的聚氰基丙烯酸丁酯（PBCA）纳米粒。通过NMR、H-1 NMR和X-射线衍射证实了HA和PBCA之间的化学偶联。当铈浓度为0.8 mmol/L、HA分子量为18，000 Da时，不同HA/BCA比的纳米颗粒尺寸为291-325 nm。抗癌模型药物紫杉醇（紫杉醇）被包裹在带负电荷的纳米颗粒中，最大包裹效率为90%。体外释药实验表明，HA修饰后可有效降低10 h内的突释，并在随后的188 h内提供持续释放。溶血试验和MTT试验表明，HA涂层可显著降低细胞毒性。细胞摄取表明肉瘤-180（S-180）细胞对HA-PBCA纳米颗粒的摄取比PBCA纳米颗粒高9.5倍。在静脉内施用至S-180荷瘤小鼠后，装载M的HA-PBCA纳米颗粒比装载PTX的PBCA纳米颗粒或PTX注射液在肿瘤生长抑制方面更有效。因此，HA-PBCA纳米粒可能是一种有效和安全的载体，用于疏水性抗癌药物的全身给药。(C)2009爱思唯尔有限公司版权所有。
The hyaluronic acid (HA) coated poly(butyl cyanoacrylate) (PBCA) nanoparticles were synthesized through radical polymerization of butyl cyanoarylate (BCA) initiated by cerium ions in the presence of HA. The chemical coupling between HA and PBCA was demonstrated by MR, H-1 NMR and X-ray diffraction. The sizes of the nanoparticles with different HA/BCA ratios were 291-325 nm at cerium concentration of 0.8 mmol/L and HA molecular weight of 18,000 Da. Paclitaxel (PTX), a model anticancer drug, was encapsulated in negatively charged nanoparticles with a maximal encapsulation efficiency of 90%. In vitro release demonstrated that HA modification could effectively reduce the initial burst release in the first 10 h and provide a sustained release in the subsequent 188 h. As evidenced by the hemolysis assay and MTT assay, HA coating could significantly reduce the cytotoxicity. Cellular uptake indicated that uptake of HA-PBCA nanoparticles by Sarcoma-180 (S-180) cells was 9.5-fold higher than that of PBCA nanoparticles. M-loaded HA-PBCA nanoparticles were more potent in tumor growth suppression than PTX-loaded PBCA nanoparticles or PTX injection following intravenous administration to S-180 tumor bearing mice. Therefore, the HA-PBCA nanoparticles could be an effective and safe vehicle for systemic administration of hydrophobic anticancer drugs. (C) 2009 Elsevier B.V. All rights reserved.